Alkyne-Val-Cit-PAB, CAS 2748039-76-9, acts as a cleavable linker for Antibody-Drug Conjugates (ADCs). It features an alkyne group, a Valine-Citrulline (Val-Cit) dipeptide, and a self-immolative para-aminobenzyloxycarbonyl (PAB) moiety. This combination helps release the drug selectively inside target cells, boosting the effectiveness of delivery.
Key Features
- Cleavable Val-Cit Dipeptide: The Val-Cit sequence responds to lysosomal enzymes like cathepsin B, which triggers drug release inside cells. It stays stable in human plasma, lowering the risk of off-target effects.
- Alkyne Group: The terminal propargyl (alkyne) quickly links to azide-containing biomolecules using Click Chemistry, allowing for versatile applications.
- Self-Immolative PAB Moiety: When the Val-Cit is cleaved, the PAB ensures the drug releases efficiently, enhancing delivery to target cells.
- Stability in Circulation: The linker remains intact in the bloodstream, so the drug reaches its target without premature release.
Applications
- Antibody-Drug Conjugates (ADCs): Links cytotoxic drugs to antibodies, providing targeted cancer therapy by directing the drug straight to tumor cells.
- Targeted Drug Delivery: Enables selective release in areas with high protease activity, such as tumors or lysosomes.
- Bioconjugation: The alkyne group allows fast Click Chemistry with azide-modified biomolecules, expanding conjugation possibilities.
Advantages
- Precise Drug Release: The Val-Cit sequence releases the drug only when specific lysosomal enzymes like cathepsin B are present, commonly found in tumor cells.
- High Stability: Remains stable in plasma, reducing unwanted release and potential side effects.
- Flexible Conjugation: The alkyne group easily attaches to various biomolecules through Click Chemistry, making it highly adaptable.
Alkyne-Val-Cit-PAB offers a reliable approach for designing ADCs and targeted therapies. It combines stability in the bloodstream with selective release inside cells, leading to more effective treatment results.
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